title: Synthesis, characterisation, and in vitro anticancer activity of curcumin analogues bearing pyrazole/pyrimidine ring targeting EGFR tyrosine kinase.
abstract: In search of potential therapeutics for cancer, we described herein the synthesis, characterization, and in vitro anticancer activity of a novel series of curcumin analogues. The anticancer effects were evaluated on a panel of 60 cell lines, according to the National Cancer Institute (NCI) screening protocol. There were 10 tested compounds among 14 synthesized compounds, which showed potent anticancer activity in both one-dose and 5-dose assays. The most active compound of the series was 3,5-bis(4-hydroxy-3-methylstyryl)-1H-pyrazole-1-yl(phenyl)methanone which showed mean growth percent of -28.71 in one-dose assay and GI₅₀ values between 0.0079 and 1.86 µM in 5-dose assay.
authors.affiliation: Department of Pharmaceutical Chemistry, Maharishi Arvind College of Pharmacy, Ambabari, Jaipur, Rajasthan 302 023, India.
authors.forename: Mohamed Jawed
authors.initials: MJ
authors.lastname: Ahsan
authors.forename: Habibullah
authors.initials: H
authors.lastname: Khalilullah
authors.forename: Sabina
authors.initials: S
authors.lastname: Yasmin
authors.forename: Surender Singh
authors.initials: SS
authors.lastname: Jadav
authors.forename: Jeyabalan
authors.initials: J
authors.lastname: Govindasamy
mesh_terms: D001665:Binding Sites / Q000187:drug effects; D045744:Cell Line, Tumor / Q000187:drug effects; D018360:Crystallography, X-Ray; D003474:Curcumin / Q000008:administration & dosage* / Q000031:analogs & derivatives / Q000138:chemical synthesis*; D066246:ErbB Receptors / Q000037:antagonists & inhibitors / Q000737:chemistry* / Q000378:metabolism; D006801:Humans; D062105:Molecular Docking Simulation; D047428:Protein Kinase Inhibitors / Q000008:administration & dosage* / Q000138:chemical synthesis; D011720:Pyrazoles / Q000008:administration & dosage / Q000138:chemical synthesis; D011743:Pyrimidines / Q000008:administration & dosage / Q000138:chemical synthesis
chemical_list: D047428:Protein Kinase Inhibitors; D011720:Pyrazoles; D011743:Pyrimidines; C031280:pyrazole; C512478:EGFR protein, human; D066246:ErbB Receptors; D003474:Curcumin; C030986:pyrimidine